Reabhlaid

Ainm Ceimigeach:

1-(2-(3-((4-carbamoylpiperidin-1-yl)methyl)-N-methylbenzamido)ethyl)piperidin-4-yl [1,1'-biphenyl]-2-ylcarbamate

Còd SMILES:

O=C(OC1CCN(CCN(C))C(C2=CC=C(CN3CCC(C(N)=O)CC3)C=C2)=O)CC1)NC4=CC=CC=C4C5=CC=CC= C5

Còd InChi:

InChI=1S/C35H43N5O4/c1-38(34(42)29-13-11-26(12-14-29)25-40-19-15-28(16-20-40)33(36)41)) 23-24-39-21-17- 30(18-22-39)44-35(43)37-32-10-6-5-9-31(32)27-7-3-2-4-8-27/h2-14,28, 30H, 15-25H2,1H3,(H2,36,41)(H,37,43)

iuchair InChi:

FYDWDCIFZSGNBU-UHFFAOYSA-N

Facal-luirg:

Revefenacin, TD-4208, GSK-1160724, TD4208, TD 4208, GSK1160724, GSK 1160724, 864750-70-9

Solubility:Soluble ann an DMSO

Stòradh:0 - 4 ° C airson geàrr-ùine (làithean gu seachdainean), no -20 ° C airson ùine fhada (mìosan).

Tuairisgeul:

In Vitro: Is e na Kis de revefenacin 0.42, 0.32, 0.18, 0.56, agus 6.7 nM aig gabhadan daonna M1, M2, M3, M4 agus M5, fa leth. Ann am measadh gnìomh, thathas a’ sealltainn gu bheil revefenacin na antagonist gnìomh le cuibhreannan casg coltach ri ceangal Ki. Bidh Revefenacin cuideachd a’ cur bacadh air giorrachadh air a bhrosnachadh le agonist de ullachadh fàinne tracheal iomallach muc ghuine le dàimh de 0.1 nM, coltach ris an tomhas M3 tagradh Ki [1]. Ann am Vivo: Ann an coin le anesthetized, bidh revefenacin, còmhla ri tiotropium agus glycopyrronium, a’ toirt a-mach casg seasmhach air bronchoconstriction air a bhrosnachadh le acetylcholine airson suas ri 24 uairean. Ann am radain le anesthetized, tha revefenacin inhalaichte a’ taisbeanadh broncho-dhìon 24-uair a tha an urra ri dòs an aghaidh bronchoconstriction air a bhrosnachadh le methacholine. Is e an comas measta 24-uair 45.0 µg / mL agus tha na comasan bronchoprotective air an cumail suas às deidh 7 latha de dòsachadh aon-latha[2].

Targaid: MaChR